With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13544-43-9,6-(Trifluoromethyl)-1H-indole,as a common compound, the synthetic route is as follows.
In a round-bottomed flask, 1.0 g of 6-trifluorom- ethylindole (5.40 mmol; 1.00 eq) were dissolved in 10 mE of acetone (10.00 mE), 0.68 g of potassium hydroxide (12.15 mmol; 2.25 eq) were added to this dark orange solution and then the mixture was stirred at RT for 15 mm and 672 tE of iodomethan (10.80 mmol; 2.00 eq) were added. The reaction mixture was stirred at RT for 20 h. The reaction medium was then taken up with water and extracted with ethyl acetate. The organic phase was washed once with a saturated NaC1 solution, dried over MgSO4 and concentrated under reduced pressure. The residue was purified by flash chromotography (l3iolage 50 g silica 30 microns adsorption on silica in dichloromethane) using a cyclohexane/ethyl acetate gradient of 99/1 to 90/10. The fractions containing the targeted product were combined and then evaporated under reduced pressure to give 835 mg of 1 -methyl-6-(trifluoromethyl)indole.10575] Yld: 78%. ?H NMR (300 MHz, DMSO-d5) oeppm 3.88 (s, 3H)6.56 (d, J=3.1 Hz, 1H) 7.30 (d, J=8.3 Hz, 1H) 7.57 (d, J=3.0Hz, 1H) 7.74 (d, J=8.3 Hz, 1H) 7.86 (s, 1H).
As the paragraph descriping shows that 13544-43-9 is playing an increasingly important role.
Reference£º
Patent; INVENTIVA; BOUBIA, Benaissa; MASSARDIER, Christine; GUILLIER, Fabrice; POUPARDIN, Olivia; TALLANDIER, Mireille; AMAUDRUT, Jerome; BONDOUX, Michel; FEENSTRA, Roelof Williem; VAN DONGEN, Maria Johana Petronella; (207 pag.)US2017/66717; (2017); A1;,
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